2024
Phosphoenolpyruvate carboxykinase-2 (PCK2) is a therapeutic target in triple-negative breast cancer
Gunasekharan V, Lin H, Marczyk M, Rios-Hoyo A, Campos G, Shan N, Ahmed M, Umlauf S, Gareiss P, Raaisa R, Williams R, Cardone R, Siebel S, Kibbey R, Surovtseva Y, Pusztai L. Phosphoenolpyruvate carboxykinase-2 (PCK2) is a therapeutic target in triple-negative breast cancer. Breast Cancer Research And Treatment 2024, 208: 657-671. PMID: 39177932, DOI: 10.1007/s10549-024-07462-z.Peer-Reviewed Original ResearchMetabolic fluxTriple-negative breast cancerReduced metabolic fluxMDA-MB-231 cellsCell growth in vitroEnzyme assays in vitroMDA-MB-231Potential small molecule inhibitorsPyruvate carboxylaseGrowth in vitroSmall molecule inhibitorsIn silico screeningEnzyme assaysAssay in vitroEnzymatic assayCell lines in vitroEnzyme activityGrowth inhibitory activityBT-549Breast cancerIn vitro screeningBreast cell lines in vitroPhosphoenolpyruvateSignificant growth inhibitory activityLines in vitro
2014
TP53 mutation‐correlated genes predict the risk of tumor relapse and identify MPS1 as a potential therapeutic kinase in TP53‐mutated breast cancers
Győrffy B, Bottai G, Lehmann-Che J, Kéri G, Őrfi L, Iwamoto T, Desmedt C, Bianchini G, Turner NC, de Thè H, André F, Sotiriou C, Hortobagyi GN, Di Leo A, Pusztai L, Santarpia L. TP53 mutation‐correlated genes predict the risk of tumor relapse and identify MPS1 as a potential therapeutic kinase in TP53‐mutated breast cancers. Molecular Oncology 2014, 8: 508-519. PMID: 24462521, PMCID: PMC5528634, DOI: 10.1016/j.molonc.2013.12.018.Peer-Reviewed Original ResearchConceptsBreast cancerTP53 mutation statusPrognostic valueBC cellsMutation statusER-negative breast cancerDifferent BC cell linesFuture clinical trialsSignificant prognostic markerPotential therapeutic targetBC cell linesType of treatmentNeoadjuvant chemotherapyBC patientsClinical behaviorPrognostic markerClinical trialsConventional chemotherapyEstrogen receptorPotent small molecule inhibitorsTumor relapseSmall molecule inhibitorsTherapeutic targetClinical relevanceTP53 status
2009
Amplification of fibroblast growth factor receptor-1 in breast cancer and the effects of brivanib alaninate
Shiang CY, Qi Y, Wang B, Lazar V, Wang J, Fraser Symmans W, Hortobagyi GN, Andre F, Pusztai L. Amplification of fibroblast growth factor receptor-1 in breast cancer and the effects of brivanib alaninate. Breast Cancer Research And Treatment 2009, 123: 747-755. PMID: 20024612, DOI: 10.1007/s10549-009-0677-6.Peer-Reviewed Original ResearchMeSH KeywordsAlanineAntineoplastic AgentsBreast NeoplasmsCell Line, TumorCell ProliferationComparative Genomic HybridizationDose-Response Relationship, DrugFemaleFibroblast Growth Factor 2Gene AmplificationGene DosageGene Expression ProfilingGene Expression Regulation, NeoplasticHumansInhibitory Concentration 50Mitogen-Activated Protein Kinase 1Mitogen-Activated Protein Kinase 3PhosphorylationProto-Oncogene Proteins c-aktReceptor, Fibroblast Growth Factor, Type 1RNA, MessengerSignal TransductionTriazinesConceptsFibroblast growth factor receptor 1Growth factor receptor 1Breast cancer cell linesBreast cancerFactor receptor 1Cancer cell linesKinase activityProtein overexpressionReceptor 1Cell linesCopy numberDirect anti-proliferative effectsGene expression profilingHuman breast cancerTyrosine kinase activityAnti-angiogenic effectsMDA-MB-361Small molecule inhibitorsAnti-proliferative effectsGrowth inhibitionDNA copy numberProtein expression levelsBrivanib treatmentFGFR-1 mRNANormal copy number